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    • 11. 发明授权
    • Tetrahydro-azepinoquinolines
    • 四氮唑腈
    • US3987047A
    • 1976-10-19
    • US520965
    • 1974-11-05
    • Gerhart GrissRudolf HurnausWolfgang GrellRobert SauterRichard Reichl
    • Gerhart GrissRudolf HurnausWolfgang GrellRobert SauterRichard Reichl
    • C07D471/04C07D491/14C07D491/147
    • C07D471/04C07D491/14Y10S514/96Y10S514/966
    • Compounds of the formula ##SPC1##Wherein ##EQU1## where R.sub.1 is hydrogen, straight or branched aliphatic acyl of 1 to 12 carbon atoms, methoxy-substituted straight or branched aliphatic acyl of 1 to 12 carbon atoms, benzoyl, halo-benzoyl, carbalkoxy of 2 to 7 carbon atoms, carbcycloalkoxy of 4 to 7 carbon atoms, benzyl, methylbenzyl, phenylsulfonyl, halo-phenylsulfonyl, tolylsulfonyl, alkenyl of 2 to 6 carbon atoms, phenyl, trifluoroacetyl, amidino, amido, thioamido, phenoxycarbonyl, benzyloxycarbonyl, methylsulfonyl or--B -- XwhereB is straight or branched alkylene of 1 to 6 carbon atoms, andX is hydrogen, hydroxyl, methoxy, carboxyl, cyano, dimethylaminocarbonyl, morpholino-carbonyl or carbalkoxy of 2 to 6 carbon atoms,R.sub.2 is hydrogen, hydroxyl, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkanoyloxy of 1 to 3 carbon atoms, alkoxycarbonyloxy of 2 to 4 carbon atoms, amino, dimethylamino, morpholino or halogen,R.sub.3 is hydrogen, halogen, hydroxyl, carboxyl, straight or branched alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms, phenyl-alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms -- alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms, hydroxymethyl, phenyl, phenoxy, amino, pyrrolidino or morpholino,R.sub.4, r.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen, halogen, methyl, hydroxyl, methoxy, cyano, amino, nitro, trifluoromethyl, carboxyl, acetyl or carbalkoxy of 2 to 4 carbon atoms, or any two of R.sub.4, R.sub.5 and R.sub.6 together are methylenedioxy, andX.sub.1 and X.sub.2 are hydrogen or together form a double bond,6-N-oxides thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anoretics.
    • 17. 发明授权
    • Phenylethanolamines, their use as pharmaceuticals and as performance
enhancers in animals
    • 苯乙醇胺,它们用作药物和作为动物中的性能增强剂
    • US5232946A
    • 1993-08-03
    • US572969
    • 1990-08-20
    • Rudolf HurnausManfred ReiffenRobert SauterWolfgang GrellEckhard Rupprecht
    • Rudolf HurnausManfred ReiffenRobert SauterWolfgang GrellEckhard Rupprecht
    • A61K31/13A61K31/135A61K31/16A61K31/19A61K31/195A61K31/215A61K31/22A61K31/275A61K31/40A61P3/00A61P43/00C07C213/00C07C215/30C07C215/32C07C215/48C07C215/54C07C215/68C07C217/56C07C217/62C07C221/00C07C225/16C07C227/00C07C229/38C07C233/43C07C237/30C07C253/30C07C255/53C07C255/59
    • C07C255/00C07C229/38
    • The invention relates to new phenylethanolamines of general formula ##STR1## wherein A represents a straight-chained or branched alkylene group,B represents a bond, an alkylene group, a carbonyl or hydroxymethylene group,R.sub.1 represents a hydrogen atom, a halogen atom or a trifluoromethyl group,R.sub.2 represents a hydrogen atom or an amino group,R.sub.3 represents a cyano group, a hydrogen, chlorine or bromine atom andR.sub.4 represents a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, carboxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl group or an alkoxy group substituted in the end position by a carboxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, hydroxy, alkoxy, amino, alkylamino, dialkylamino, pyrrolidino, piperidino or hexamethyleneimino group,the optical isomers and diastereoisomers and acid addition salts thereof.The new compounds of formula I, the optical isomers and diastereoisomers and acid addition salts thereof, particularly the physiologically acceptable acid addition salts thereof with inorganic or organic acids, have valuable pharmacological properties, namely an effect on the metabolism, preferably the effect of lowering blood sugar and reducing body fat and they may also be used as performance enhancers in animals.The new compounds of general formula I above may be prepared by methods known per se.
    • PCT No.PCT / EP88 / 01083 Sec。 371日期1990年8月20日 102(e)1990年8月20日日期PCT提交1988年11月29日PCT公布。 WO90 / 06299 PCT出版物 日本1990年6月14日。本发明涉及通式为(I)的新型苯乙醇胺,其中A表示直链或支链亚烷基,B表示键,亚烷基,羰基或羟基亚甲基,R1 表示氢原子,卤原子或三氟甲基,R 2表示氢原子或氨基,R 3表示氰基,氢,氯或溴原子,R 4表示氢或卤素原子,烷基,羟基, 烷氧基羰基,烷氧基羰基,氨基羰基,烷基氨基羰基或二烷基氨基羰基或由羧基,烷氧基羰基,氨基羰基,烷基氨基羰基,二烷基氨基羰基,羟基,烷氧基,氨基,烷基氨基,二烷基氨基,吡咯烷子基,哌啶子基或六亚甲基亚氨基取代的烷氧基。 光学异构体和非对映异构体及其酸加成盐。 式I的新化合物,其光学异构体和非对映异构体及其酸加成盐,特别是其与无机或有机酸的生理上可接受的酸加成盐具有有价值的药理学性质,即对代谢的影响,优选降低血液的作用 糖和减少身体脂肪,并且它们也可以用作动物中的性能增强剂。 上述通式I的新化合物可以通过本身已知的方法制备。
    • 20. 发明授权
    • Tetrahydro-benzthiazoles, the preparation thereof and their use as
intermediate products or as pharmaceuticals
    • 四氢 - 苯并噻唑,其制备方法及其作为中间产物或药物的用途
    • US4731374A
    • 1988-03-15
    • US810947
    • 1985-12-19
    • Gerhart Griss, deceasedRudolf HurnausWalter KobingerLudwig PichlerRudolf BauerJoachim MierauDieter HinzenGunter Schingnitz
    • Gerhart Griss, deceasedRudolf HurnausWalter KobingerLudwig PichlerRudolf BauerJoachim MierauDieter HinzenGunter Schingnitz
    • A61K31/425C07D277/82
    • C07D277/82
    • This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.
    • 本发明涉及通式为(I)的新的四氢苯并噻唑,其中R 1表示氢原子,烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基,而上述苯基核 可各自被1或2个卤素原子取代,R2表示氢原子或烷基,R3表示氢原子,烷基,环烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基 基团可以被氟里酰,氯或溴原子取代,R4表示氢原子,烷基,烷基或烯基,或者R3和R4与它们之间的氮原子一起代表吡咯烷子基,哌啶子基, 六亚甲基亚氨基或吗啉代基,其对映异构体及其酸加成盐。 上述通式I的化合物,其中R1或R3基团或R1和R3两个基团之一表示酰基,是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。